Spot-on formulations for combating parasites

Abstract

In particular this invention provides for spot-on compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise:(1) a composition comprising(A) an effective amount of a 1-phenylpyrazole derivative; and / or(B) an effective amount of a macrocyclic lactone antihelmintic or antiparasitic agent;(2) an acceptable liquid carrier vehicle; and(3) optionally, a crystallization inhibitor.The invention also provides for a method of treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal or bird an effective amount of a composition according to the present invention.

Description

RELATED APPLICATIONS[0001]This application is a division of application Ser. No. 09 / 376,736, filed Aug. 17, 1999, U.S. Pat. No. 6,426,333, which is a continuation-in-part of application U.S. Ser. No. 09 / 271,470, filed Mar. 17, 1999, U.S. Pat. No. 6,482,425 which in turn is a continuation-in-part of copending International Application PCT / FR97 / 01548 having an international filing date of Sep. 15, 1997, and designating the U.S. and claiming priority from French Application No. 96 / 11446, filed Sep. 19, 1996. Reference is also made to: U.S. applications Ser. Nos. 08 / 719,942, filed Sep. 25, 1996, 08 / 692,430, filed Aug. 5, 1996, 08 / 863,182, filed May 27, 1997, 08 / 692,113, filed Aug. 5, 1996, 08 / 863,392, filed May 27, 1997, and 08 / 891,047, filed Jul. 10, 1997; French Application No. 97 03709, filed Mar. 26, 1997; and PCT / FR98 / 00601. All of the above-mentioned applications, as well as all documents cited herein and documents referenced or cited in documents cited herein, are hereby incorpor...

AI Technical Summary

Benefits of technology

[0024]The invention provides for spot-on formulations for the treatment or prophylaxis of parasites of mammals and birds, and in particular, cats, dogs, horses, chickens, sheep and cattle with the aim of ridding these hosts of all the parasites commonly encountered by birds and mammals. The invention also provides for effective and lasting destruction of ectoparasites, such as fleas, ticks, itch mites and lice, and of endoparasites, nematodes, such as filariae, and roundworms of the digestive tract of animals and humans.

[0030](3) optionally, a crystallization inhibitor.The invention also provides for an easy method of treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal or bird an effective amount of a formulation according to the present invention.

[0032]This invention further provides for formulations which, when applied locally, will diffuse over the entire body of the host and then dry, without crystallizing, and which do not affect the appearance of the coat after drying by, for example, leaving crystals or making the coat sticky. This has the further advantage in animals which groom themselves of not being orally ingested, where the therapeutic agent might not be well tolerated orally or might interact with other therapeutic agents.

[0033]The very high effectiveness of the method and of the formulations according to the invention provides not only for a high instantaneous effectiveness but also for an effectiveness of very long duration after the treatment of the animal.

Problems solved by technology

Animals such as mammals and birds are often susceptible to parasite infestations.

Fleas are a particular problem because not only do they adversely affect the health of the animal or human, but they also cause a great deal of psychological stress.

Similarly, ticks are also harmful to the physical and psychological health of the animal or human.

However, the most serious problem associated with ticks is that they are the vector of pathogenic agents, agents which cause diseases in both humans and animal.

Occasionally, these toxins are fatal to the host.

Moreover, galls are particularly difficult to combat since there are very few active substances which act on these parasites and they require frequent treatment.

Likewise, farm animals are also susceptible to parasite infestations.

Ticks, such as Boophilus microplus, are particularly difficult to control because they live in the pasture where the farm animals graze.

These parasites cause severe economic losses in pigs, sheep, horses, and cattle as well as affecting domestic animals and poultry.

However the results of these insecticides is not always satisfactory because of, for example, the development of resistance by the parasite to the therapeutic agent, as is the case, for example, with carbamates, organophosphorus compounds and pyrethroids.

Moreover, there is at the present time no truly effective method for controlling both ticks and helminths and less still an effective way of controlling the set of parasites indicated above.

Fipronil is particularly, but not exclusively, effective against fleas and ticks.

While it is known in the art that it is sometimes possible to combine various parasiticides in order to broaden the antiparasitical spectrum, it is not possible to predict, α priori, which combinations will work for a particular animal or disease state.

For this reason, the results of various combinations is not always successful and there is a need in the art for more effective formulations which may be easily administered to the animal.

The effectiveness of formulations comprising 1-N-phenylpyrazole derivatives and macrolide lactone antihelmintic or parasitic agents, such as avermectins, ivermectins and milbemycin, against an endoparasite or an ectoparasite in a specific host is especially difficult to predict because of the numerous and complex host-parasite interactions.

However, this patent application does not provide specific guidance to the skilled artisan on how to formulate a 1-N-pyrazole derivative with an avermectin or milbemycin type compound, let alone how to formulate a spot-on composition comprising these compounds.

Moreover, the application does not indicate which specific parasites are susceptible to what specific combination.

However, as discussed in U.S. Pat. No. 5,045,536, a large number of solvent systems described in the art provide formulations for localized topical application which cause irritancy or toxicity to the host.

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